4.5 Article

Design and modular parallel synthesis of a MCR derived α-helix mimetic protein-protein interaction inhibitor scaffold

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 6, 页码 1740-1743

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.11.102

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protein interaction antagonist; cancer; Bc1 family; apoptosis; multicomponent reaction; isocyanide

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A terphenyl alpha-helix mimetic scaffold recognized to be capable of disrupting protein-protein interactions was structurally morphed into an easily amenable and versatile multicomponent reaction (MCR) backbone. The design, modular in-parallel library synthesis, initial cell based biological data, and preliminary in vitro screening for the disruption of the Bcl-w/Bak protein-protein interaction by representatives of the MCR derived scaffold are presented. (C) 2006 Published by Elsevier Ltd.

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